Influence of polymer molecular weight on in vitro dissolution behavior and in vivo performance of celecoxib:PVP amorphous solid dispersions

Research output: Contribution to journalJournal articlepeer-review

Standard

Influence of polymer molecular weight on in vitro dissolution behavior and in vivo performance of celecoxib:PVP amorphous solid dispersions. / Knopp, Matthias Manne; Nguyen, Julia Hoang; Becker, Christian; Francke, Nadine Monika; Jørgensen, Erling B; Holm, Per; Holm, René; Mu, Huiling; Rades, Thomas; Langguth, Peter.

In: European Journal of Pharmaceutics and Biopharmaceutics, Vol. 101, 04.2016, p. 145-51.

Research output: Contribution to journalJournal articlepeer-review

Harvard

Knopp, MM, Nguyen, JH, Becker, C, Francke, NM, Jørgensen, EB, Holm, P, Holm, R, Mu, H, Rades, T & Langguth, P 2016, 'Influence of polymer molecular weight on in vitro dissolution behavior and in vivo performance of celecoxib:PVP amorphous solid dispersions', European Journal of Pharmaceutics and Biopharmaceutics, vol. 101, pp. 145-51. https://doi.org/10.1016/j.ejpb.2016.02.007

APA

Knopp, M. M., Nguyen, J. H., Becker, C., Francke, N. M., Jørgensen, E. B., Holm, P., Holm, R., Mu, H., Rades, T., & Langguth, P. (2016). Influence of polymer molecular weight on in vitro dissolution behavior and in vivo performance of celecoxib:PVP amorphous solid dispersions. European Journal of Pharmaceutics and Biopharmaceutics, 101, 145-51. https://doi.org/10.1016/j.ejpb.2016.02.007

Vancouver

Knopp MM, Nguyen JH, Becker C, Francke NM, Jørgensen EB, Holm P et al. Influence of polymer molecular weight on in vitro dissolution behavior and in vivo performance of celecoxib:PVP amorphous solid dispersions. European Journal of Pharmaceutics and Biopharmaceutics. 2016 Apr;101:145-51. https://doi.org/10.1016/j.ejpb.2016.02.007

Author

Knopp, Matthias Manne ; Nguyen, Julia Hoang ; Becker, Christian ; Francke, Nadine Monika ; Jørgensen, Erling B ; Holm, Per ; Holm, René ; Mu, Huiling ; Rades, Thomas ; Langguth, Peter. / Influence of polymer molecular weight on in vitro dissolution behavior and in vivo performance of celecoxib:PVP amorphous solid dispersions. In: European Journal of Pharmaceutics and Biopharmaceutics. 2016 ; Vol. 101. pp. 145-51.

Bibtex

@article{b59ac3bb3b5642bb91b36e5727082d71,
title = "Influence of polymer molecular weight on in vitro dissolution behavior and in vivo performance of celecoxib:PVP amorphous solid dispersions",
abstract = "In this study, the influence of the molecular weight of polyvinylpyrrolidone (PVP) on the non-sink in vitro dissolution and in vivo performance of celecoxib (CCX):PVP amorphous solid dispersions were investigated. The dissolution rate of CCX from the amorphous solid dispersions increased with decreasing PVP molecular weight and crystallization inhibition was increased with increasing molecular weight of PVP, but reached a maximum for PVP K30. This suggested that the crystallization inhibition was not proportional with molecular weight of the polymer, but rather there was an optimal molecular weight where the crystallization inhibition was strongest. Consistent with the findings from the non-sink in vitro dissolution tests, the amorphous solid dispersions with the highest molecular weight PVPs (K30 and K60) resulted in significantly higher in vivo bioavailability (AUC0-24h) compared with pure amorphous and crystalline CCX. A linear relationship between the in vitro and in vivo parameter AUC0-24h indicated that the simple non-sink in vitro dissolution method used in this study could be used to predict the in vivo performance of amorphous solid dispersion with good precision, which enabled a ranking between the different formulations. In conclusion, the findings of this study demonstrated that the in vitro and in vivo performance of CCX:PVP amorphous solid dispersions were significantly controlled by the molecular weight of the polymer.",
author = "Knopp, {Matthias Manne} and Nguyen, {Julia Hoang} and Christian Becker and Francke, {Nadine Monika} and J{\o}rgensen, {Erling B} and Per Holm and Ren{\'e} Holm and Huiling Mu and Thomas Rades and Peter Langguth",
note = "Copyright {\textcopyright} 2016 Elsevier B.V. All rights reserved.",
year = "2016",
month = apr,
doi = "10.1016/j.ejpb.2016.02.007",
language = "English",
volume = "101",
pages = "145--51",
journal = "European Journal of Pharmaceutics and Biopharmaceutics",
issn = "0939-6411",
publisher = "Elsevier",

}

RIS

TY - JOUR

T1 - Influence of polymer molecular weight on in vitro dissolution behavior and in vivo performance of celecoxib:PVP amorphous solid dispersions

AU - Knopp, Matthias Manne

AU - Nguyen, Julia Hoang

AU - Becker, Christian

AU - Francke, Nadine Monika

AU - Jørgensen, Erling B

AU - Holm, Per

AU - Holm, René

AU - Mu, Huiling

AU - Rades, Thomas

AU - Langguth, Peter

N1 - Copyright © 2016 Elsevier B.V. All rights reserved.

PY - 2016/4

Y1 - 2016/4

N2 - In this study, the influence of the molecular weight of polyvinylpyrrolidone (PVP) on the non-sink in vitro dissolution and in vivo performance of celecoxib (CCX):PVP amorphous solid dispersions were investigated. The dissolution rate of CCX from the amorphous solid dispersions increased with decreasing PVP molecular weight and crystallization inhibition was increased with increasing molecular weight of PVP, but reached a maximum for PVP K30. This suggested that the crystallization inhibition was not proportional with molecular weight of the polymer, but rather there was an optimal molecular weight where the crystallization inhibition was strongest. Consistent with the findings from the non-sink in vitro dissolution tests, the amorphous solid dispersions with the highest molecular weight PVPs (K30 and K60) resulted in significantly higher in vivo bioavailability (AUC0-24h) compared with pure amorphous and crystalline CCX. A linear relationship between the in vitro and in vivo parameter AUC0-24h indicated that the simple non-sink in vitro dissolution method used in this study could be used to predict the in vivo performance of amorphous solid dispersion with good precision, which enabled a ranking between the different formulations. In conclusion, the findings of this study demonstrated that the in vitro and in vivo performance of CCX:PVP amorphous solid dispersions were significantly controlled by the molecular weight of the polymer.

AB - In this study, the influence of the molecular weight of polyvinylpyrrolidone (PVP) on the non-sink in vitro dissolution and in vivo performance of celecoxib (CCX):PVP amorphous solid dispersions were investigated. The dissolution rate of CCX from the amorphous solid dispersions increased with decreasing PVP molecular weight and crystallization inhibition was increased with increasing molecular weight of PVP, but reached a maximum for PVP K30. This suggested that the crystallization inhibition was not proportional with molecular weight of the polymer, but rather there was an optimal molecular weight where the crystallization inhibition was strongest. Consistent with the findings from the non-sink in vitro dissolution tests, the amorphous solid dispersions with the highest molecular weight PVPs (K30 and K60) resulted in significantly higher in vivo bioavailability (AUC0-24h) compared with pure amorphous and crystalline CCX. A linear relationship between the in vitro and in vivo parameter AUC0-24h indicated that the simple non-sink in vitro dissolution method used in this study could be used to predict the in vivo performance of amorphous solid dispersion with good precision, which enabled a ranking between the different formulations. In conclusion, the findings of this study demonstrated that the in vitro and in vivo performance of CCX:PVP amorphous solid dispersions were significantly controlled by the molecular weight of the polymer.

U2 - 10.1016/j.ejpb.2016.02.007

DO - 10.1016/j.ejpb.2016.02.007

M3 - Journal article

C2 - 26899127

VL - 101

SP - 145

EP - 151

JO - European Journal of Pharmaceutics and Biopharmaceutics

JF - European Journal of Pharmaceutics and Biopharmaceutics

SN - 0939-6411

ER -

ID: 160402931